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Chemically modified dendrimers

Chemically modified dendrimers description/claims

This application claims the benefit of U.S. Provisional Application Ser. No. 60/945,815, filed on Jun. 22, 2007, which is incorporated herein by reference in its entirety.

This invention relates to dendrimers, compositions comprising the dendrimers, and methods of use thereof, for example, in the treatment of inflammatory disorders such as arthritis.

There are many forms of arthritis, including rheumatoid arthritis, psoriatic arthritis, and osteoarthritis. The most common form of arthritis, osteoarthritis, is also known as degenerative joint disease and can occur following trauma to the joint, following an infection of the joint or simply as a result of aging. There is emerging evidence that abnormal anatomy may contribute to early development of osteoarthritis.

Osteoarthritis is a condition where low-grade inflammation can result in pain in the joints, for example, pain caused by wearing of the cartilage that covers and acts as a cushion inside joints. As the bone surfaces become less well protected by cartilage, a subject can experience pain upon simply bearing weight, for example walking or standing. Due to decreased movement caused by pain, regional muscles may atrophy, and ligaments may become more lax.

Arthritis is generally treated with NSAIDs, local injections of glucocorticoid or viscosupplements based on hyaluronan, salt of hyaluronic acid or derivative thereof, such as a solution of hyaluronan, and in some cases, with surgery, for example, joint replacement surgery. There is currently no cure for arthritis.

Applicants have discovered that certain compounds can be used to treat MMP (e.g., MMP-1, -3, or -13) mediated disorders including inflammatory disorders, such as arthritis. The compounds are dendrimers having a plurality of terminal acyl urea moieties. The term “dendrimer,” when used herein, refers to a polymer moiety comprised of branched repeating units that radiate out from a central atom, multifunctional moiety, or cluster of atoms. Each branched repeating unit terminates with a terminal moiety. An example of a dendrimer is shown below:

wherein I represents the central atom, multifunctional moiety, or cluster of atoms and Z represents the terminal moieties of the branched repeating units.

In one aspect, the invention features a dendrimer, the dendrimer comprising a plurality of branched repeating units radiating out from a central atom, multifunctional moiety, or cluster of atoms, wherein each repeating unit comprises a terminal moiety, and wherein at least about 5% of the terminal moieties include a urea of formula (I)

wherein

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